A61P29/02

5-HT3 receptor antagonists

The present invention provides 5-HT3 receptor antagonists of Formula (I): ##STR00001##
which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Compositions and methods for inhibiting expression of the ALAS1 gene

The invention relates to double-stranded ribonucleic acid (dsRNA) compositions targeting the ALAS1 gene, and methods of using such dsRNA compositions to alter (e.g., inhibit) expression of ALAS1.

COLCHICINE SALICYLATE DERIVATIVES AND METHODS OF TREATMENT
20180318221 · 2018-11-08 · ·

Pharmaceutical compositions of colchicine salicylate, including once-a-day orally administered formulations are provided. Method of treating and/or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

P2X4 RECEPTOR ANTAGONIST

Compounds represented by the following general formula (I), which has a P2X4 receptor antagonistic activity (in the formula, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, a halogen atom, and the like, X represents C or N, Y represents N or C(O), provided that when X is C, Y represents N, and when X is N, Y represents C(O), the double line consisting of the solid line and the broken line represents a single bond or double bond, n represents an integer of 0 to 6, Z represents O, S, or an atomic bond, and A represents benzene ring, pyridine ring, and the like).

##STR00001##

TRICYCLIC SPIRO COMPOUND

A medicinal agent for the prevention and/or treatment of diseases caused by EP.sub.4 receptor activation. A compound having antagonistic activity against the EP.sub.4 receptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EP.sub.4 receptor for the prevention and/or treatment of diseases caused by EP.sub.4 receptor activation.

##STR00001##

Methods and compositions for treating pain

Methods for treating pain such as fibromyalgia, comprising administering to a subject in need thereof an effective amount of an adenosine analog, wherein the adenosine analog may be a compound of Formula (I): ##STR00001## (I), or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising the adenosine analog for use in treating pain (e.g., fibromyalgia), optionally further comprising Substance P (SP), are also provided.

METHODS OF ADMINISTERING PIRFENIDONE THERAPY
20180311221 · 2018-11-01 ·

The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.

ANTI-EGFRvIII ANTIBODIES AND USES THEREOF

The present invention provides antibodies that bind to the class III variant of EGFR (EGFRvIII) and methods of using the same. According to certain embodiments, the antibodies of the invention bind human EGFRvIII with high affinity. The antibodies of the invention may be fully human antibodies. The invention includes anti-EGFRvIII antibodies conjugated to a cytotoxic agent, radionuclide, or other moiety detrimental to cell growth or proliferation. The antibodies of the invention are useful for the treatment of various cancers.

11,13-modified saxitoxins for the treatment of pain

Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): ##STR00001##
where R.sup.1, X.sup.1 and X.sup.3 are as described herein.

Boron-based prodrug strategy for increased bioavailability and lower-dosage requirements for drug molecules containing at least one phenol (or aromatic hydroxyl) group
10112962 · 2018-10-30 · ·

Boron-based prodrugs of phenol- or aromatic hydroxyl group-containing therapeutic molecules (original drugs), uses thereof, and methods of making the same, are provided for achieving, for example, improved bioavailability, prolonged retention (e.g., in a circulatory system) and, in particular, significantly lowered therapeutically effective dosage in order to reduce adverse effects while maintaining the desired therapeutic effects of the original drugs.